Synthesis and biological evaluation of 3-(1H-indol-3-yl)pyrazole-5-carboxylic acid derivatives.
Synthesis and biological evaluation of 3-(1H-indol-3-yl)pyrazole-5-carboxylic acid derivatives.
复制标题
3-(1H-吲哚-3-基)吡唑-5-羧酸衍生物的合成和生物学评价。
DOI：
10.1007/s12272-011-0301-2
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发表时间：
2011
影响因子：
6.7
通讯作者：
Huo,Lingyan
中科院分区：
文献类型：
--
作者：
Zhang,Datong;Wang,Guangtian;Tan,Chubing;Xu,Weiren;Pei,Yuan;Huo,Lingyan
A series of novel compounds bearing a 3-(1H-indol-3-yl)pyrazole-5-carboxylic acid nucleus were synthesized. Analytical and spectral data confirmed the structures of the new compounds. The structures of the regioisomers in this series were determined by1H-NMR spectra. The title compounds were evaluated for their endothelin-1 antagonist activities. In thein vitrofunctional assay, compounds23, 24, 28and29exhibited significant efficacy at the concentration of 1 μg/mL, and compounds5b, 5c, 26and28were as potent as the positive control bosentan at high concentration. In the experiment to assess prevention of endothelin-1-induced sudden death in mice, compound5bshowed comparable activity to bosentan, and30was more potent than bosentan. The final compounds were also screened for antibacterial activity against four Gram-positive and -negative bacteria. Some of the tested compounds showed weak antibacterial activity.
